GBR 12935 is an inhibitor of dopamine uptake that binds to the dopamine transporter (Kd = 27.2 nM).1,2 It is selective for the dopamine transporter over the serotonin and norepinephrine transporters (Kds = 940 and 310 nM, respectively).1 In mice, it increases locomotor activity, but not stereotypic behavior, when administered at a dose of 10 mg/kg but induces gnawing at levels similar to other indirect dopamine agonists with an ED50 value of 17.1 mg/kg.2,3
1.Tatsumi, M., Groshan, K., Blakely, R.D., et al.Pharmacological profile of antidepressants and related compounds at human monoamine transportersEur. J. Pharmacol.340(2-3)249-258(1997) 2.Tirelli, E., and Witkin, J.M.Differential effects of direct and indirect dopamine agonists on the induction of gnawing in C57Bl/6J miceJ. Pharmacol. Exp. Ther.273(1)7-15(1995) 3.Tolliver, B.K., and Carney, J.M.Comparison of cocaine and GBR 12935: Effects on locomotor activity and stereotypy in two inbred mouse strainsPharmacol. Biochem. Behav.48(3)733-739(1994)